Navigation Links
Experimental cancer pharmaceuticals under trial
Date:10/23/2007

A potent and selective inhibitor of the mitotic kinesin CENP-E (GSK923295A) demonstrates a novel mechanism of inhibiting tumor cell proliferation and shows activity against a broad panel of human tumor cell lines in vitro: Abstract A 111.

A first-in-class, targeted investigational therapy specifically designed to inhibit a single protein that functions only during cell division shows potent activity in a broad range of cancer cell lines, say researchers from GlaxoSmithKline. Because the compound is so specifically targeted, it may help reduce some of the more common toxic side effects of chemotherapy, they say.

The experimental drug, GSK923295A, inhibits the mitotic kinesin centromere-associated protein E (CENP-E), which is required during mitosis, the process by which a cell duplicates its genetic information in order to generate two, identical, daughter cells. The resulting mitotic arrest can lead to apoptosis, or cell death. A characteristic of CENP-E inhibition is the presence of misaligned or lagging chromosomes within cells attempting to replicate.

Investigators were able to observe lagging chromosomes in most tumor cells treated with GSK923295A. These effects are rarely observed in untreated cells, said the studys lead investigator, David Sutton, B.Sc., associate director of biology, within the Oncology division of GlaxoSmithKline in Collegeville, Pa. GlaxoSmithKline funded the study.

Although CENP-E is expressed in all dividing cells, GSK923925A is more likely to affect rapidly dividing cancer cells, Sutton says. Furthermore, because of the very low expression of CENP-E in non-dividing cells such as neurons, GSK923295A may not cause the peripheral nerve damage often seen with chemotherapy treatments such as taxanes and vinca alkaloids, which also inhibit mitosis, he says.

Studies conducted in animal models have shown complete tumor regression in some cancer types, says Sutton. In preclinical tests conducted in 214 solid and 85 hematological tumor cell lines, sensitivity to GSK923295A was seen in 16 out of 17 breast tumor cell lines, 20 out of 25 colon cancer lines, 24 out of 26 lung cancer lines, 11 out of 11 ovarian cancer lines, and six out of six prostate cancer lines, he says. Additionally, laboratory analysis suggests that anti-tumor activity might be achieved with minimal suppression of the bone marrow, which could reduce the typical myelosuppression (reduction in production of blood cells) seen with chemotherapy treatment, he says.

It is a big leap from doing laboratory experiments to understanding what will happen in patients, but we think it is very encouraging that this first-in-class drug candidate shows both broad activity and the potential for enhanced tolerability in preclinical studies, Sutton said. GSK923295A, a small molecule drug given intravenously, is now being evaluated in a Phase I clinical trial in patients with advanced solid tumors. It was discovered and optimized by GSK, in partnership with Cytokinetics Inc.


'/>"/>

Contact: Greg Lester
greg.lester@aacr.org
267-646-0554
American Association for Cancer Research
Source:Eurekalert

Related medicine news :

1. Experimental treatment for Ebola Virus Shows promising results in mice
2. FDA approves Phase 0 trial which tests experimental drugs on humans
3. Experimental drug to fight flu
4. Experimental SARS Vaccine
5. Experimental vaccine for shingles is effective
6. Experimental Blood Test May Spot Heart Attack Risk, Study Says
7. Five AIDS Patients To Receive Experimental Anti-retroviral Drugs
8. TMC 114 and 125 experimental drugs to be tested on four HIV patients
9. Protection against HIV and Herpes is possible with the Experimental Microbicide
10. Experimental Therapy Effective Against Malignant Melanoma in Horses
11. Experimental Alzheimer’s Drug curbs the disease in mic
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:9/26/2017)... ... September 26, 2017 , ... Atmosera , a ... Management as a Service (RMaaS) to automate the deployment of websites and ... companies, e-tailers, and web development agencies who want to improve time-to-revenue with a ...
(Date:9/26/2017)... ... , ... As the holiday season nears, best deals online website, ... to find tips and stories for products and services savings. With a lot of ... deals. The deals are organized by categories so can easily find what you’re looking ...
(Date:9/26/2017)... Falls Church, VA (PRWEB) , ... September 26, 2017 , ... ... FDAnews and Cerulean Associates LLC **, Dec. 5-6, 2017 – Arlington, VA, http://www.fdanews.com/fdadataintegrity ... its investigators: “If initial findings indicate the firm’s electronic records may not be trustworthy ...
(Date:9/26/2017)... ... September 26, 2017 , ... Autism Learning ... Northern Colorado. Aspire Autism, A Division of Autism Learning Partners, will be the ... Aspire provides center based Autism services in Broomfield and will continue to operate ...
(Date:9/26/2017)... ... September 26, 2017 , ... The Organizing Committee ... tactical plans for Pittcon 2018. As of July 1, Adrian C. Michael, Ph.D. ... named vice president, Charles Gardner, (ChemImage Corporation) and selected chairs. , ...
Breaking Medicine News(10 mins):
(Date:9/7/2017)... BioLife Solutions , Inc. (NASDAQ: BLFS ), the ... and tissue hypothermic storage and cryopreservation freeze ... and CEO, will be presenting at two investment conferences in ... th Annual Global Investment Conference on Tuesday, September 12th, ... conference is being held at the New York Palace Hotel ...
(Date:9/6/2017)... , Sept. 6, 2017 Eli Lilly ... it will present new data for galcanezumab and lasmiditan, ... of the International Headache Society (IHC) taking place Sept. ... Lilly will highlight new, long-term data from an ... doses of galcanezumab (120 mg and 240 mg) for ...
(Date:9/5/2017)... Oramed Pharmaceuticals Inc. (NASDAQ: ORMP ) (TASE: ... on the development of oral drug delivery systems, announced ... the U.S. Food and Drug Administration (FDA) regarding ORMD-0801, ... At the meeting, the FDA gave ... ORMD-0801, would be a Biologics License Application (BLA).  Such ...
Breaking Medicine Technology: